All Photos(1)
Synonym(s):
VprBP Inhibitor, B32B3, Vpr Binding protein Inhibitor
Empirical Formula (Hill Notation):
C19H17N5S
Recommended Products
Assay
≥98% (HPLC)
Quality Level
form
powder
potency
500 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light yellow
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell permeable, potent, selective, and ATP-competitive inhibitor of Vpr (HIV-1) binding protein (VprBP) that preferentially targets cancer cells expressing VprBP and blocks phosphorylation of H2A at Thr120 (IC50 = 500 nM in DU-145 human prostate cancer cells) and reduces cell proliferation. However, it has minimal effect on normal human prostate MLC cells lacking VprBP. Exhibits over 100-fold greater selectivity for VprBP over a panel of 33 other protein kinases. Shown to reduce xenograft tumor progression in nude mice injected with DU-145 cells (~5 mg/kg, i.p. twice a week for 3 weeks). Displays moderately desirable pharmacokinetic properties with t1/2= 7 h and Cmax of 1 µM.
A cell permeable, potent, selective, and ATP-competitive inhibitor of Vpr (HIV-1) binding protein (VprBP) that preferentially targets cancer cells expressing VprBP and blocks phosphorylation of H2A at Thr120 (IC50 = 500 nM in DU-145 human prostate cancer cells) and reduces cell proliferation. However, it has minimal effect on normal human prostate MLC cells lacking VprBP. Exhibits over 100-fold greater selectivity for VprBP over a panel of 33 other protein kinases. Shown to reduce xenograft tumor progression in nude mice injected with DU-145 cells (~5 mg/kg, i.p. twice a week for 3 weeks). Displays moderately desirable pharmacokinetic properties with t1/2= 7 h and Cmax of 1 µM.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
VprBP
VprBP
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kim, K., et al. 2013. Mol. Cell.52, 459.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service